L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE

中文名称:

L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE

中文同义词:

(L-3-反式-(丙基氨基甲酰基)环氧乙烷-2-羰基)-L-异亮氨酰-L-脯氨酸;CATHEPSIN B抑制剂(CA-074)

英文名称:

CA-074

英文同义词:

N-(L-3-TRANS-PROPYLCARBAMOYL-OXIRANE-2-CARBONYL)-ILE-PRO-OH;L-trans-Epoxysuccinyl(propylamide)-Ile-Pro;N-(L-3-trans-PropylcarbaMoyl-oxirane-2-carbonyl)-Ile-Pro-OH, CA-074, L-trans-Epoxysuccinyl(propylaMide)-Ile-Pro-OH;INHIBITOR FOR CATHEPSIN B;CATHEPSIN B INHIBITOR III;CA-074;[L-3-TRANS-(PROPYLCARBAMOYL)OXIRANE-2-CARBONYL]-L-ISOLEUCYL-L-PROLINE;(L-3-TRANS-(PROPYLCARBAMYL)OXIRANE-2-CARBONYL)-L-ISOLEUCYL-L-PROLINE

CAS号:

134448-10-5

分子式:

C18H29N3O6

分子量:

383.44

EINECS号:

200-258-5

相关类别:

细胞生物学试剂;peptides;Pepetides;Inhibitor

Mol文件:

134448-10-5.mol

沸点 

728.9±60.0 °C(Predicted)

密度 

1.267±0.06 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

Soluble in methanol at 1mg/ml. Also soluble in DMSO or ethanol.

形态

solid

酸度系数(pKa)

3.43±0.20(Predicted)

生物活性

CA-074是组织蛋白酶B (cathepsin B) 的有效抑制剂， Ki 值为2 to 5 nM。

靶点

Ki: 2 to 5 nM (Cathepsin B)

体外研究

CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug. CA-074 inhibits cathepsin B with a K i of 2 to 5 nM, whereas the initial K i s for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L.

体内研究

Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity. Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys.

WGK Germany 

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